Biochem/physiol Actions
Activator of ether-a-go-go-related (hERG) potassium channel. Used in the treatment of congestive heart failure.
PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activator, a representative in the series of structural analogs; PD-118057 at 10 μM leads to a 111% current increase in rabbit ventricular wedge (in comparison RPR260243 leads to only a 15% increase at the same concentration);PD-118057, unlike RPR260243, does not have a major effect on gating or kinetic properties of this channel. PD-118057prevents and reverses QT interval prolongation; Compounds such as PD-118057 may offer new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure
Features and Benefits
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| color | light yellow |
| solubility | DMSO: 9 mg/mL |
| storage temp. | −20°C |
| SMILES string | OC(=O)c1ccccc1Nc2ccc(CCc3ccc(Cl)c(Cl)c3)cc2 |
| InChI | 1S/C21H17Cl2NO2/c22-18-12-9-15(13-19(18)23)6-5-14-7-10-16(11-8-14)24-20-4-2-1-3-17(20)21(25)26/h1-4,7-13,24H,5-6H2,(H,25,26) |
| InChI key | ZCQOSCDABPVAFB-UHFFFAOYSA-N |
